Pharmacological properties of lidamidine hydrochloride (WHR-1142A) , a novel antidiarrheal agent
Mir, G.N.; Sperow, J.W.; Riley, R.L.; Alioto, R.L.; Nuss, G.W.; Chou, B.J.; Yelnosky, J.
Arzneimittel-Forschung 28(8a): 1466-1470
1978
ISSN/ISBN: 0004-4172 PMID: 582538 Document Number: 131770
1-(2',6'-Dimethylphenyl)-3-amidinourea hydrochloride (WHR-1142A, lidamidine hydrochloride), a potent, unique antidiarrheal agent, was tested for other pharmacological properties. It inhibited gastric acid secretion in both 4-h and 22-h pylorus-ligated rats and reduced mortality and gastric ulcer severity in the latter test. WHR-1142A also exhibited local anesthetic activity in the rabbit corneal reflex and guinea pig intradermal wheal tests and reverisbly blocked conduction in isolated frog nerves. Low doses of WHR-1142A increased plasma glucose concentration in fasted mice and rats and prolonged the hyperglycemia in response to a glucose meal. WHR-1142A showed mild diuretic activity but had no anti-inflammatory or antibacterial activity. The acute oral LD50 of WHR-1142A was 260 (208,328) mg/kg in male mice, 267 (212,336) mg/kg in male rats and 160 130,197) mg/kg in female rats.